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Pharmacokinetics
Ch. 1,3,4
80
Nursing
Graduate
08/23/2014

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Term
WHAT IS PHARMACOKINETICS?
Definition
WHAT THE BODY DOES TO THE DRUG
Term
WHAT DOES PHARMACOKINETICS ADDRESS?
Definition
ABSORPTION, DISTRIBUTION, METABOLISM, AND ELIMINATION (ADME)
Term
WHAT IS A TERM THAT ALSO DETERMINES THE TIMING OF EFFECT (ONSET, PEAK AND DURATION) OF A DRUG?
Definition
PHARMACOKINETICS
Term
WHAT ARE FACTORS THAT CAN ALTER THE PHARMACOKINETICS OF A DRUG?
Definition
BIOAVAILABILITY; AGE, GENETICS, BODY COMPOSITION; RENAL, HEPATIC, AND CARDIAC FUNCTION
Term
WHAT MAJOR VEIN RAPIDLY ABSORBS MEDICATIONS FROM THE ENTERNAL (SUBLINGUAL/BUCCAL) ROUTE?
Definition
SVC
Term
WHY DOES THE SUBLINGUAL/BUCAL ROUTE HAVE MINIMAL HEPATIC FIRST-PASS?
Definition
BECAUSE IT GOES TO THE SVC INSTEAD OF THE PORTAL VEIN FROM THE STOMACH
Term
ARE PO MEDICATIONS EXPOSED TO HEPATIC FIRST-PASS?
Definition
YES, BECAUSE IT GOES THROUGH THE PORTAL VEIN AND TO THE LIVER
Term
DOES RECTAL ADMINISTRATION OF MEDICATION PRODUCE LOCAL, SYSTEMIC, OR BOTH EFFECTS?
Definition
BOTH
Term
WHY DOES LOWER RECTAL ADMINISTRATION HAVE LIMITED HEPATIC FIRST PASS ABSORPTION?
Definition
BECAUSE THE MEDICATIONS LEAD INTO THE IVC
Term
WHAT IS FIRST-PASS HEPATIC EFFECT?
Definition
DRUGS THAT ARE ABOSRBED FROM THE GUT ENTER THE HEPATIC PORTAL BEIN, ENTER THE LIVER AND ARE METABOLIZED INTO POORLY ACTIVE COMPOUNDS WITH LOW BIOAVAILABILITY. IT CAN ALSO BE EXPLAINED AS A PHENOMENON OF DRUG METABOLISM WHEREBY THE CONCENTRATION OF A DRUG IS GREATLY REDUCED BEFORE IT REACHES THE SYSTEMIC CIRCULATION.
Term
WHAT IS UNIQUE ABOUT THE IV ROUTE OF MEDICATION ADMINISTRATION? 4 ANSWERS
Definition
1)IT BYPASSES THE PROCESS OF ABSORPTION
2)RAPID ONSET
3)ALLOWS TIGHT CONTROL OVER DOSE DELIVERED (THEREFORE EFFECT PRODUCED)
4)MOST WIDELY USED METHOD OF DRUG DELIVERY IN ANESTHESIA
Term
WHAT IS A BIG FACTOR RELATED TO IM ABSOPTION RATE?
Definition
DEPENDENT ON BLOOD FLOW TO MUSCLE AND SOLUTION IN WHICH IS IT ADMINISTERED.
Term
NAME SOME DRUGS USED IN ANESTHESIA THAT ARE ADMINISTERED SQ?
Definition
INSULIN, TERBUTALINE FOR PRETERM LABOR (RELAXES THE UTERUS R/T PRECURSOR TO EPI), AND EPI
Term
WHAT 2 COMPONENTS MAKE UP NEURAXIAL?
Definition
EPIDURAL AND INTRATHECAL (SPINAL)
Term
WHERE IS THE SITE OF ACTION OF EPIDURAL AND SPINAL MEDICATIONS?
Definition
NERVE ROOTS, ROOTLETS, AND SPINAL CORD
Term
WHERE EXACTLY IS THE EPIDURAL SPACE?
Definition
THE SPACE SURROUNDING THE DURA MATER OF THE SPINAL CORD. ** LAYERS ** EPIDURAL, DURA MATER, ARACHNOID, SUBARACHNOID SPACE (WHERE CSF IS), AND PIA MATER *DAP*
Term
WHAT IS A BIG CONCERN WITH EPIDURAL ADMINSTRATION OF MEDICATIONS?
Definition
SYSTEMIC UPTAKE RELATED TO THE VASCULATURE
Term
WHAT MUST TRANSDERMAL DRUGS BE RELATED TO LIPO/HYDRO, TO PASS THE EPIDERMAL LAYER?
Definition
LIPID SOLUBLE, LIPOPHILIC
Term
ALONG WITH IV ADMINISTRATION WHAT OTHER FORM OF ADMINISTRATION HAS JUST AS RAPID ONSET?
Definition
INHALATIONAL
Term
WHAT IS PERINEURAL?
Definition
INJECTION OR INFUSION OF MEDICATION AT OR NEAR A NERVE TO PROVIDE LOSS OF SENSATION.
Term
WHAT 3 STEPS TAKE PLACE IN ABSORPTION?
WHAT 2 ROUTES DOES ABSORPTION NOT APPLY TO?
Definition
DRUGS MUST PASS FROM THE SITE OF ADMINISTRATION, THEN INTO THE CIRUCULATION, THEN TO THE TARGET SITE. DOESN'T APPLY TO IV OR TRANSDERMAL( R/T LOCAL)
Term
WHAT ARE THE 3 COMMON MEANS OF ABSORPTION?
Definition
PASSIVE DIFFUSION, ACTIVE TRANSPORT, AND FACILITATED TRANSPORT.
Term
DESCRIBE PASSIVE DIFFUSION. WHAT TYPE OF MOLECULES DO NOT UNDERGO PASIVE DIFFUSION?
Definition
MOST COMMON TYPE OF ABSORPTION IN WHICH DRUGS MOVE DOWN A CONCENTRATION GRADIENT ALTHOUGH IT IS DEPENDENT ON THE PERMIABILITY OF THE CELL MEMBRANE. CHARGED MOLECULES DO NOT UNDERGO PASSIVE DIFFUSION.
Term
WHAT DOES FICK'S LAW OF DIFFUSION STATE IN RELATION TO PASSIVE DIFFUSION? WHAT INCREASES AND DECREASES DIFFSION?
Definition
THE RATE OF DIFFUSION IS INCREASED BY LARGE CONCENTRATION GRADIENT AND SURFACE AREA AVAILABLE FOR DIFFUSION. THE RATE OF DIFFUSION IS DECREASED BY MEMBRANE THICKNESS (LENGTH) AND LARGE MOLECULAR SIZE
Term
WHAT IS THE FORMULA FOR FICK'S LAW OF DIFFUSION?
Definition
FLUX (MOLECULES PER UNIT TIME) =
(C1-C2) X (AREA X PERMEABILITY COEFFICIENT / THICKNESS)
Term
WHAT IS UNIQUE ABOUT PASSIVE DIFFUSION IN RELATION TO LIPID OR AQUEOUS DIFFUSION? WHICH DIFFUSION IS LIMITED TO MOLECULAR SIZE AND WHY?
Definition
IT CAN BE EITHER LIPID OR AQUEOUS DEPENDING ON WHAT PART OF THE CELL MEMBRANE THE PARTICLE DIFFUSES THROUGH. AQUEOUS DIFFUSION IS LIMITED BY MOLECULAR SIZE -MOST DRUGS ARE TOO LARGE TO DIFFUSE THROUGH THE PORES.
Term
WHAT IS ACTIVE TRANSPORT? CAN IT MOVE ACROSS A CONCENTRATION GRADIENT?
Definition
A TYPE OF TRANSPORT INRELATION TO ABSORPTION IN WHICH ENERGY IN THE FORM OF ATP IS NEEDED TO MOVE DRUGS ACROSS THE CELL MEMBRANE. IT CAN MOVE ACROSS A CONCENTRATION GRADIENT RELATED TO THE USE OF ENERGY.
Term
WHAT IS FACILITATED TRANSPORT? WHAT DOES IT HAVE TO FOLLOW? WHAT IS IT FASTER THAN?
Definition
IT REQUIRES A CARRIER MOLECULE ALTHOUGH DOESN'T REQUIRE ENERGY. IT HAS TO FOLLOW A CONCENTRATION GRADIENT. ITS FASTER THAN PASSIVE DIFFUSION.
Term
DESCRIBE DISTRIBUTION.
Definition
WHEN DRUGS ARE *DELIVERED* TO ORGANS AND TISSUE SO THAT THEY CAN EXERT THE DESIRED EFFECT.
Term
WHAT ARE THE FACTORS AFFECTING DISTRUCTION? (5 FACTORS)
Definition
BLOOD FLOW, PLASMA PROTEIN BINDING, MOLECULAR SIZE, LIPID SOLUBILITY, ELECTRICAL CHARGE.
Term
WHAT ARE THE VESSEL RICH GROUPS (VRG) IN WHICH THEY REPRESENT 10% OF BODY MASS ALTHOUGH 75% OF CARDIAC OUTPUT?
Definition
LUNGS, HEART, BRAIN, LIVER, AND KIDNEY.
Term
WHAT % OF BODY MASS IS THE MUSCLE AND HOW MUCH CO DOES IT RECIEVE?
Definition
50% AND IT RECEIVES 20% OF CO.
Term
WHAT % OF BODY MASS IS THE FAT GROUP AND HOW MUCH CO DOES IT RECEIVE?
Definition
20% IN NORMAL ADULTS, BUT ONLY RECEIVES ABOUT 5% OF CO.
Term
WHERE ARE THE VESSEL POOR GROUP (VPG) AND HOW MUCH CO DO THEY RECEIVE?
Definition
BONE, CARTILAGE, AND TEETH. RECEIVES LESS THAN 1% OF CO THEREFORE NEARLY NO DRUG DELIVERY TO THESE SITES.
Term
DURING PLASMA PROTEIN BINDING WHAT PART OF THE DRUG IS AVAILABLE TO DIFFUSE TO TARGET SITES OR RESERVOIRS? WHAT HAPPENS WHEN THE FREE DRUG IS DISTRIBUTED?
Definition
THE FREE (UNBOUND) PART. WHEN THE FREE DRUG IS DISTRIBUTED, THE BOUND DRUG DISSOCIATES FROM THE PROTEIN IN ORDER TO MAINTAIN AN EQUILIBRIUM BETWEEN BOUND AND FREE DRUG IN THE PLASMA.
Term
WHAT IS THE MAIN PLASMA PROTEIN IN WHICH MOST DRUGS, ESPECIALLY ACIDS BIND TO? WHAT OTHER TYPE OF PLASMA PROTEIN DOES BASIC DRUGS BIND TO? FYI- THE DEGREE OF PROTEIN BINDING CAN AFFECT THE DISTRIBUTION AND HALF-LIFE OF A DRUG.
Definition
ALBUMIN; A-1 GLYCOPROTEIN
Term
WHEN ARE LOW ALBUMIN LEVELS TYPICALLY FOUND IN? (4 ANSWERS) WHEN ARE LOW A-1 GLYCOPROTEIN LEVELS FOUND IN? (4 ANSWERS)
Definition
ELDERLY, RENAL OR HEPATIC DISEASE, MALNUTRITION.; NEONATES, CHRONIC PAIN, SURGERY, MI
Term
DESCRIBE HOW MOLECULAR SIZE AFFECTS DISTRIBUTION.
Definition
LARGE MOLECULES (HEPARIN) ARE UNABLE TO READILY DIFFUSE ACROSS THE MEMBRANES, THEREFORE ARE NOT WIDELY DISTRIBUTED.
Term
DESCRIBE HOW LIPID SOLUBILITY AFFECTRS DISTRIBUTION.
Definition
HIGHLY LIPID SOLUBLE DRUGS MORE READILY CROSS THE CELL MEMBRANE AND DISTRIBUTE THROUGHOUT.
Term
DESCRIBE THE LIPID:AQUEOUS PARTITION COEFFICIENT.
Definition
PARTITION COEFFICIENTS ARE A MEASURE OF SOLUBILITY (THE RATIO OF THE CONCENTRATION BETWEEN 2 PARTITIONS). THE HIGHER THE LIPID:AQUEOUS PARTITION COEFFICIENT, THE MORE LIPID SOLUBLE THE DRUG IS.
Term
DESCRIBE HOW THE ELECTRICAL CHARGE AFFECTS DISTRIBUTION.
Definition
CHARGED MOLECULES DO NOT UNDERGO PASSIVE DIFFUSION AND CAN ACCUMULATE ON ONE SIDE OF THE OTHER OF A MEMBRANE.
Term
MOST DRUGS COMMONLY USED ARE WHAT IN RELATION TO WEAK/STRONG ACID/BASE? WHAT DOES THE WEAK NOTATION MEAN?
Definition
WEAK ACIDS OR WEAK BASES. THE WEAK NOTATION MEANS THA THE COMPOUND DISSOCIATES VERY EASILY (WEAK BONDS).
Term
WHAT IS AN ACID? WHAT IS THE EQUATION?
Definition
A COMPOUND THAT CAN DISSOCIATE AND RELEASE (GIVE UP, LOSE, DONATE) A HYDROGEN ION (H+). AH - A- + H+
Term
WHAT IS A BASE? WHAT IS THE EQUATION?
Definition
A COMPOUND THAT CAN *ACCEPT* A HYDROGEN ION (H+). B+H+ - BH+
Term
THE PROTONATED FORM OF AN ACID AND THE UNPROTONATED FORM OF A BASE IS WHAT?
Definition
THE NON-IONIZED FORM.
Term
WHEAT DOES IONIZED MEAN?
Definition
IONIZED IS THE SAME THING AS CHARGED. CHARGED PARTICLES ARE REPELLED BY A CELL MEMBRANE.
Term
A PROTONATED ACID OR UNPROTONATED BASE CAN CAHNGE THEIR IONIZATION HOW?
Definition
BY PICKING UP OR RELEASING A H+ DEPENDING ON THE pH OF THE ENVIRONEMENT.
Term
WHAT DETERMINES A DRUG SITE AND RATE OF ABSORPTION/DIFFUSION?
Definition
THE RATIO OF IONIZED TO NON-IONIZED FORM OF A DRUG.
Term
WHAT PART OF THE DRUG IS THE LIPID SOLUBLE FORM?
Definition
THE NON-IONIZED FORM OF A DRUG. REMEMBER LIPID SOLUBLE DRUGS ARE EASILY ABORBED AND DISTRIBUTED TO SITES OF ACTION. UNIONIZED = NON-IONIZED. LIPID SOLUBLE = LIPOPHILIC OR HYDROPHOBIC
Term
WHAT FORM OF A DRUG IS THE WATER SOLUBLE FORM.
Definition
IONIZED FORM. WATER SOLUBLE = HYDROPHILIC OR LIPOPHOBIC.
Term
WHAT IS pka? WHAT DOES IT DETERMINE?
Definition
THE DISSOCIATION CONSTANT OR IONIZATION CONSTANT. THE pka IS A *CONSTANT*, SPECIFIC TO EVERY DRUG, THAT IS USED IN THE HENDERSON-HASSELBALCH EQUATION TO DERMINES THE RATIO OF IONIZED TO UNIONIZED FORM OF A DRUG. THE pka DOESN'T CHANGE AND IS NOT THE SAME AS THE pH, BUT THE pH AFFECTS THE DRUGS ACTION DEPENDING ON THE pka AND WHEATHER THE DRUG IS A WEAK ACID OR A WEAK BASE.
Term
WHAT HAPPENS WHEN THE pka = pH? WHAT HAPPENS WHEN THE pH CHANGES?
Definition
THE RATIO OF IONIZED (WATER SOLUBLE) TO UNIONIZED (LIPID SOLUBLE) IS EQUAL. THERE IS 50% OF EACH OF THE PROTONATED VS NONPROTONATED FORM OF THE DRUG. WHEN THE pH CHANGES (REMEMBER THE pka IS CONSTANT), SO DOES THE RATIO OF IONIZED TO UNIONIZED.
Term
WHEN THE pH < pka WHAT FORM IS GREATER?
Definition
PROTONATED
Term
WHEN THE pH > pka WHAT FORM IS GREATER?
Definition
UNPROTONATED (IONIZED)
Term
DESCRIBE ION TRAPPING.
Definition
ANYTIME THERE IS A pH GRADIENT BETWEEN COMPARTMENTS (PLASMA AND INTRACELLULAR SPACE, PLASMA, AND URINE) THERE CAN BE "TRAPPING" OF A DRUG IN ITS IONIZED (WATER SOLUBLE) FORM, WHICH MEANS THAT IT CAN NO LONGER CROSS THE MEMBRANE.
Term
DESRIBE ION TRAPPING IN RELATION TO FETAL AND MATERNAL pH.
Definition
FETAL pH IS LOWER THAN MATERNAL pH...A WEAK BASE LIKE AN OPIOD OR LOCAL ANESTHETIC) IN ITS UNIONIZED (LIPID SOLUBLE) FORM IN THE MOTHER'S CIRCULATION CAN EASILY CROSS THE PLACENTAL BARRIER. ONCE IT IS EXPOSED TO THE LOWER pH OF THE FETUS, IT BECOMES IONIZED AND IS TRAPPED IN THE FETAL CIRCULATION, WHICH CAN LEAD TO ENHANCED FETAL EFFECTS.
Term
DESCRIBE HOW THE pH OF URINE CAN INVOLVE ION TRAPPING.
Definition
THE pH OF URINE CAN BE MANIPULATED IN ORDER TO TRAP A DRUG SO THAT IT IS CLEARED MORE EFFECTIVELY, ESPECIALLY IN THE CASE OF AN OVERDOSE.
Term
WEAK ACID (BARBS AND ASA) BECOME IONIZED (WATER SOLUBLE) AND TRAPPED IN BASIC URINE. WHAT IS USED TO ALKALINIZE THE URINE?
Definition
SODIUM BICARB
Term
WEAK BASES (LIDOCAINE AND AMPHETAMINE) BECOME IONIZED AND TRAPPED IN ACIDIC URINE. WHAT IS USED TO ACIDIFY THE URINE?
Definition
AMMONIUM CHLORIDE.
Term
WHAT DO WEAK ACIDS BIND TO?
Definition
POSITIVELY CHARGED IONS. EX. NA+, MG++, CA++. DRUGS THAT HAVE THESE IN THEIR NAMES ARE TYPICALLY WEAK ACIDS, EX. SODIUM THIOPENTAL
Term
WHAT DO WEAK BASES BIND TO?
Definition
NEGATIVELY CHARGED IONS (CL-, SO42-). EX LIDOCAINE, HYDROCHLORIDE, MORPHINE SULFATE
Term
NOT ALL DRUGS ARE WEAK ACIDS OR WEAK BASES... SOME ARE NEUTRAL SALTS. GIVE SOME EXAMPLES.
Definition
MAGNESIUM SULFATE, SODIUM CHLORIDE, CALCIUM CHLORIDE.
Term
NAME THE pH OF PLASMA, CSF, URINE, BREAST MILK, GASTRIC ACID, SMALL INTESTINE (DUODENUM),(ILEUM), AND LARGE INTESTINE.
Definition
PLASMA 7.35 TO 7.45, CSF 7.3, URINE 4-8, BREAST MILK 6.5-7.5, GASTRIC ACID, 1-3, DUODENUM 5-6, ILEUM 8, LARGE INTESTINE 8
Term
DESCRIBE BIOTRANSFORMATION. WHAT IS THE MAJOR SITE OF BIOTRANSFORMATION ALONG WITH OTHER SITES?
Definition
ONCE THE DRUG HAS BEEN DISTRIBUTED INTO THE PLASMA AND TISSUES, THE BODY BEGINS TO INACTIVATE THE DRUG. THE LIVER IS THE MAJOR SITE, BUT CAN ALSO BE GI TRACT, LUNGS, SKIN, KIDNEYS, OR BRAIN.
Term
WHAT IS THE END RESULT OF BIOTRANSFORMATION? CAN THE METABOLITES BE ACTIVE, INACTIVE, OR BOTH?
Definition
ALTHOUGH THERE ARE SEVERAL PHASES THE END RESULT IS ALMOST ALWAYS A POLAR, MORE WATER-SOLUBLE COMPOUND THAT IS MORE EASILY EXCRETED. THE METABOLITES CAN BE ACTIVE OR INACTIVE.
Term
WHAT ARE PRODRUGS? WHY IS IT BENEFICIAL? GIVE AN EXAMPLE.
Definition
MEDICATIONS THAT ARE ADMINISTERED IN AN INACTIVE FORM, THEN METABOLIZED INTO A BIOLOGICALLY ACTIVE COMPOUND. THE PRODRUG IS USUALLY BETTER ABSORBED THAN THE DESIRED COMPOUND. ENALAPRIL (VASOTEC) IS CONVERTED TO THE ACTIVE COMPOUND AFTER THE FIRST-PASS THROUGH THE LIVER.
Term
WHAT ARE THE 3 TYPES OF BIOTRANSFORMATION?
Definition
OXIDATIVE, HYDROLYTIC, AND REDUCTIVE
Term
DESCRIBE OXIDATIVE BIOTRANSFORMATION.
Definition
OXIDATIVE IS THE MOST COMMON TYPE OF THE PHASE I REACTION. BY DEFINITION, OXIDATIONS INVOLVES LOSS OF ELECTRONS. IT INCLUDES A CYP450 ENZYME CATALYZATION AND CYTOPLASMIC OXIDASES (ALCOHOL DEHYDROGENASE TO ETHANOL, XANTHINE OXIDASE FOR CAFFEINE AND THEOPHYLLINE, AND MONOAMINE OXIDASE FOR CATHECHOLAMINES AND PSYCHOTROPIC DRUGS).
Term
WHY IS CYP IMPORTANT?
Definition
IT INDUCES THE SPEED OF THE METABOLISM OF DRUGS THAT ARE DEPENDENT ON THIS PATHWAY FOR BIOTRANSFORMATION, RESULTING IN A SHORTER DURATION AND DECREASED EFFECTS.
Term
WHAT DO CYP INHIBITORS DO?
Definition
THEY SLOW THE METABOLISM OF DRUGS THAT USE THE CYP SYSTEM RESULTING IN EXAGGERATED EFFECTS AND A LONGER HALF-LIFE.
Term
DESCRIBE HYDROLYTIC IN TERMS OF BIOTRANSFORMATION.
Definition
MOLECULES THAT REACT WITH WATER WHICH BREAKS THE ORIGINAL MOLECULE INRO SMALLER MOLECULES. ESTERS AND AMIDES ARE HYDROLYZED BY MULTIPLE ENZYMES. "-ASE"
Term
DESCRIBE REDUCTIVE IN TERMS OF BIOTRANSFORMATION.
Definition
REDUCTION INVOLVES THE GAIN OF ELECTRONS (OPPOSITE OF OXIDATION). IT IS THE LEAST COMMON OF PHASE I REACTIONS AND CAN BE CYP ENZYME MEDIATED.
Term
MANY DRUGS CAN UNDERGO A COMBINATION OF PHASE I REACTIONS (HYDROLYTIC, REDUCTIVE, & OXIDATIVE). GIVE AN EXAMPLE OF A DRUG THAT DOES THIS?
Definition
NTG UNDERGOES REDUCTIVE HYDROLYSIS.
Term
DESCRIBE WHAT HAPPENS IN PHASE II BIOTRANSFORMATION. WHAT TYPE OF ENZYMES ARE INVOLVED?
Definition
CONJUGATION REACTIONS YIELD POLAR (AND TYPICALLY INACTIVE) COMPOUNDS THAT ARE EASILY EXCRETED. THIS CAN OCCUR WITH PARENT DRUG OR PHASE I METABOLITS. THIS TYPE OF BIOTRANSFORMATION IS OFTEN FASTER THAN CYP450 CATALYZED REACTIONS. TRANSFER ENZYMES (TRANSFERASES) ARE INVOLVED.
Term
LIST SOME COMMON REACTIONS WITH THE TRANSFERASES.
Definition
GLUCURONATE= GLUCURONIDATION (MOST COMMON), GLYCINE= GLYCINE CONJUGATION, ACETYL-COA= ACETYLATION, SULFATES= SULFATION, S-ADENSOSYLMETHIONINE= METHYLATION
Term
DESCRIBE THE HEPATIC EXTRACTION RATIO.
Definition
DRUGS THAT ARE CLEARED (METABOLIZED) BY THE LIVER ARE CATEGORIZED BY THEIR HEPATIC EXTRACTION RATIO. THE EXTRACTION RATIO = RATE OF ELIMINATION/RATE OF ENTRY. THE CLEARANCE OF A DRUG BY ANY ORGAN CANNOT EXCEED THAT ORGAN'S BLOOD FLOW, BUT SOME DRUGS ARE MORE DEPENDENT ON HEPATIC BLOOD FLOW, AND OTHERS ON ENZYMATIC METABOLISM.
Term
DESCRIBE A HEPATIC RATIO >0.7.
Definition
HIGH HEPATIC EXTRACTION RATIO. HEPATIC BLOOD FLOW HAS THE MOST EFFECT ON DRUG METABOLISM (CLEARANCE). LIVER FAILURE (WITH NORMAL BLOOD FLOW) WILL NOT SIGNIFICANTLY AFFECT CLEARANCE. THIS IS ALSO KNOWN AS PERFUSION-DEPENDENT ELIMINATION.
Term
DESCRIBE A HEPTIC EXTRACTION RATIO < 0.3.
Definition
LOW HEPATIC EXTRACTION RATIO. HEPATIC BLOOD FLOW HAS LITTLE EFECT ON DRUG METABOLISM AND ENZYMATIC PROCESSES PLAY THE MAJOR ROLE. LIVER FAILURE (REDUCED ENZYME PRODUCTION AND ACTIVITY) HAS A MAJOR EFFECT ON DRUG METABOLISM.
Term
NAME SOME DRUGS THAT HAVE A LOW HEPATIC EXTRACTION RATIO.
Definition
DIAZEPAM, LORAZEPAM, METHADONE, DILANTIN, ROCURONIUM, THEOPHYLLINE, THIOPENTAL
Term
NAME SOME DRUGS THAT HAVE A HIGH HAPTIC EXTRACTION RATIO.
Definition
BUPIVICAINE, DILTIAZEM, FENTANYL, KETAMINE, LABETOLOL, METOPROLOL, LIDOCAINE, DEMEROL, MORPHINE, NARCAN, PROPOFOL, SUFENTANIL.
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